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Antimetabolites
Antimetabolite drugs interfere with the synthesis of the building blocks of DNA (purine and pyrimidine bases or their corresponding nucleosides), disrupting DNA (and for some drugs RNA) synthesis and replication. Most of these drugs are structural analogues of the endogenous molecules or folate cofactors crucial for purine and pyrimidine biosynthesis. Antimetabolite class drugs principally target the de novo nucleotide synthetic pathways crucial for supplying the large nucleotide pools required by highly proliferating cancer cells.
efaccena - 16/03/2023 - 2:38pm
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Biological DMARDs
Biological DMARDs take the form of monoclonal antibodies (mAbs) and recombinant fusion proteins which modulate cytokine levels via mechanisms which inhibit T and B cell activation, or by directly inhibiting pro-inflammatory tumour necrosis factor alpha (TNFα). All cytokine modulators must be used under specialist supervision.
Examples currently employed for anti-rheumatic therapy include:
efaccena - 25/07/2016 - 2:22pm
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Disease-modifying anti-rheumatic drugs (DMARDs)
Different types of arthritis (rheumatic disease) are treated with different drugs. The aim of the clinician is to prescribe drugs which improve symptoms and, where possible, slow or halt progress of the condition. As their name suggests, disease-modifying anti-rheumatic drugs (DMARDs) offer benefit via the latter mechanism. Full therapeutic response to DMARDs may take several months to become evident. Early intervention with DMARD therapy is recommended to control the signs and symptoms of rheumatic disease and to limit joint damage.
efaccena - 22/07/2016 - 2:10pm
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Transporters as drug targets, and drug interactions
Monoamine reuptake transporters
efaccena - 21/03/2016 - 1:57pm
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TNF binding proteins (under construction)
TNF-α binding proteins can be monoclonal antibody in nature or can be recombinant proteins which act as circulating TNF-α receptors. To date their immunosuppressive activity is utilised in the treatment of autoimmune conditions.
Anti-TNF-α monoclonal antibodies
efaccena - 12/09/2016 - 11:09am
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Drug interactions - Excretion
Excretion interactions primarily involve changes in renal excretion. This might be due to drug-induced reduction in glomerular filtration rate (e.g. diuretic-induced dehydration, ACE inhibitors, NSAIDs). This can reduce the clearance and increase the plasma concentration of many drugs, including some with a low therapeutic index (e.g. digoxin, lithium, aminoglycoside antibiotics). Less commonly, interactions may be due to competition for a common tubular organic anion transporters (e.g. methotrexate excretion may be inhibited by competition with NSAIDs).
smaxwell - 30/12/2015 - 10:33am
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Dihydrofolate reductase inhibitors
Dihydrofolate reductase (DHFR) inhibitors reduce the production of folate (folic acid) required by rapidly dividing cells to make thymine for DNA synthesis.
efaccena - 08/03/2016 - 9:20am
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Therapy optimization
Patients with a given disease may differ dramatically in the desired and undesired effects of one and the same standard drug therapy. Extreme examples are:
efaccena - 24/03/2016 - 9:43am